The aims of this work are to develop new methods for organic synthesis and to examine applications of this methodology to the efficient preparation of medicinally interesting compounds. In particular methods to effect carbon-nitrogen and carbon-oxygen bond formation are proposed. The development of new synthetic methods is of central importance to the development of organic synthesis in particular and organic chemistry in general. The availability of general and predictable means by which to assemble large numbers of small molecules in both a specific as well as a combinatorial fashion is key to the uncovering of new lead structures in drug discovery. Moreover, the ability to quickly generate a diverse set of analogs of the initial lead compounds is essential for the rapid arrival at compounds with improved pharmacological profiles. Included in this work is the development of techniques that can lead to the ready availability of a wide collection of heterocyclic compounds. These compounds are the building blocks of medicinal chemistry and the pharmaceutical industry. The described methodology could have an immediate impact on the efficient access to a variety of important molecules, be they lead compounds in drug discovery or analogs of the initial leads that possess a better pharmacological profile.